BYL719 free base · Synonyms: Alpelisib

Alpelisib is a potent and selective PI3Kα inhibitor.

For research use only. Not for human or veterinary use.

Target PI3Kα

Research area Infection Neurological Disease Metabolic Disease Cancer

Purity >99% Stock Inquire

Data Sheet SDS COA

BYL719 structure

CAS No.: 1217486-61-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 485.00	BP-02122-500mg	In stock	Get quote
1 g	USD 765.00	BP-02122-1g	In stock	Get quote
5 g	USD 1,585.00	BP-02122-5g	In stock	Get quote

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Description

Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

Biological activity

In Vitro Alpelisib (0-5 μM; 14 d) significantly inhibits the clonal growth of MCF-7 and T47D breast cancer cells in 2D colony formation assays[1]. Alpelisib (5 μM; 5 d) reduces the mammosphere formation efficiency of MCF-7 and T47D breast cancer stem cell-like (BCSC-like) cells in a dose-dependent manner[1]. Alpelisib (0-10 μM; 10 d) significantly reduces the spheroid diameter of MCF-7 and T47D breast cancer stem cell-like (BCSC-like) cells in 3D culture systems, and inhibits their stem cell properties and drug resistance[1]. Alpelisib (1 μM; 24 h) significantly reduces the protein levels of the stem cell markers Nanog, Sox2, and OCT3/4 in MCF-7 and T47D breast cancer stem-like cells (BCSC-like cells)[1]. Alpelisib (10 μM; 10 d) inhibits adipogenesis, thereby attenuating adipocyte differentiation of primary LipPD1 lipoma cells in 2D culture systems and reducing the volume of 3D LipPD1 lipospheres[2]. Combination treatment with Alpelisib (10 μM; 4 d) and a 1 μM SGK3 inhibitor (VPS34-IN1 (HY-12795) or SGK3-IN) produces enhanced antiproliferative activity in Alpelisib GMP-resistant MCF7R and T47DR breast cancer cells, with a synergistic effect observed for the Alpelisib+SGK3-IN combination[3]. In Vivo Alpelisib (50 mg/kg; i.p.; daily) exerts partial antitumor activity against alpelisib-resistant MCF7R breast cancer xenografts, with maximum efficacy achieved when combined with SGK3 knockdown[3]. Alpelisib (50 mg/kg; i.p.; daily) exerts partial antitumor activity against alpelisib-resistant T47DR breast cancer xenografts, with maximum efficacy achieved when combined with SGK3 knockdown[3]. Alpelisib (25 mg/kg; p.o.; daily; 4 weeks) significantly inhibits tumor growth, reduces tumor cell proliferation, and increases tumor cell apoptosis in a PIK3CA-mutant gastric cancer xenograft model with 100% survival of treated mice over 4 weeks[4].

Identifiers

SMILES: CC1=C(SC(NC(=O)N2CCC[C@H]2C(N)=O)=N1)C1=CC(=NC=C1)C(C)(C)C(F)(F)F
InChIKey: STUWGJZDJHPWGZ-LBPRGKRZSA-N

Specifications

MW (average): 441.4700
Formula: C₁₉H₂₂F₃N₅O₂S
CAS No.: 1217486-61-7
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Yu L, et al. Effects of BYL-719 (alpelisib) on human breast cancer stem cells to overcome drug resistance in human breast cancer. Front Pharmacol. 2024;15:1443422. Published 2024 Oct 14.

[2]. Kirstein AS, et al. The Novel Phosphatidylinositol-3-Kinase (PI3K) Inhibitor Alpelisib Effectively Inhibits Growth of PTEN-Haploinsufficient Lipoma Cells. Cancers (Basel). 2019;11(10):1586. Published 2019 Oct 17.

[3]. Kang T, et al. The SGK3/GSK3β/β-catenin signaling promotes breast cancer stemness and confers resistance to alpelisib therapy. Int J Biol Sci. 2025;21(6):2462-2475. Published 2025 Mar 19.

[4]. Kim KJ, et al. PI3K-targeting strategy using alpelisib to enhance the antitumor effect of paclitaxel in human gastric cancer. Sci Rep. 2020;10(1):12308. Published 2020 Jul 23.

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